05May 2023
A Novel Oral Macrocyclic Peptide Inhibits Binding of PCSK9 to the Low-Density Lipoprotein Receptor

A Novel Oral Macrocyclic Peptide Inhibits Binding of PCSK9 to the Low-Density Lipoprotein Receptor

The study developed an oral inhibitor for PCSK9, a protein that inhibits the removal of LDL cholesterol from the bloodstream. The researchers used novel mRNA display screening technology to identify a macrocyclic peptide, MK-0616, with high affinity and selectivity for PCSK9. The safety, pharmacokinetics, and pharmacodynamics of MK-0616 were evaluated in Phase 1 clinical trials with healthy adults and those taking statins. MK-0616 showed promising results with significant reductions in free, unbound plasma PCSK9 and LDL cholesterol, indicating its potential as an effective cholesterol-lowering therapy.

  • #cardiology

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